Cytochrome P450 Inhibitor
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Polθ-IN-10
0 ImagesCat. No.: HY-181611CAS No.: 3068829-46-6Polθ-IN-10 is an orally active Polθ-pol inhibitor (with a human IC50 of 1.3 nM) that exhibits oral bioavailability in mice and rats. Polθ-IN-10 binds to the allosteric site of Polθ-pol, disrupts the microhomology-mediated end-joining DNA repair pathway, and inhibits CYP2C9 (IC50=1.63 μM). Polθ-IN-10 selectively inhibits the proliferation of HR-deficient cancer cells and induces apoptosis. Polθ-IN-10 is applicable to the research of HR-deficient cancers.
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Tetrahydropiperine (Standard)
0 ImagesTetrahydropiperine (Standard) is the analytical standard of Tetrahydropiperine (HY-N4205). This product is intended for research and analytical applications. Tetrahydropiperine is an orally effective, selective inhibitor of NF-κB and MAPKs, and an activator of the PI3K/Akt/mTOR pathway. Tetrahydropiperine reduces the production of pro-inflammatory cytokines such as TNF-α, IL-6, and nitric oxide (NO) by inhibiting the nuclear translocation of NF-κB and the phosphorylation of MAPKs such as ERK, JNK, and p38. At the same time, Tetrahydropiperine inhibits excessive autophagy by activating the PI3K/Akt/mTOR pathway, protecting neurons from oxidative damage. Tetrahydropiperine has anti-inflammatory, anti-apoptotic, and neuroprotective effects, and is mainly used in the study of inflammatory diseases (such as endotoxemia, arthritis) and neurological diseases such as ischemic stroke.
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(R)-(+)-Aminoglutethimide L-Tartrate
0 ImagesCat. No.: HY-W739700CAS No.: 57344-88-4Synonyms: d-Aminoglutethimide L-Tartrate(R)-(+)-Aminoglutethimide (L-Tartrate) is an inhibitor of aromatase. (R)-(+)-Aminoglutethimide inhibits androstenedione with a Ki value of 0.3 μM.
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Oxolamine
0 ImagesOxolamine (SKF-9976) is an orally active antitussive. Oxolamine can inhibit CYP2B1/2. Oxolamine has anti-inflammatory effects on the respiratory organs of guinea pigs. Oxolamine increases the AUC of Warfarin (HY-B0687) and prolongs its terminal half-life. Oxolamine can be used in respiratory disease research.
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Antifungal agent 122
0 ImagesCat. No.: HY-168210CAS No.: 3054212-80-2Antifungal agent 122 (compound 201) is a potent and broad-spectrum antifungal agent. Antifungal agent 122 prevents fungal phase transition and the formation of fungal biofilm. Antifungal agent 122 inhibits CYP3A4-M and CYP3A4-T enzyme activity with IC50 values of 2.11, 4.53 µM. Antifungal agent 122 shows no cytotoxicity.
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Abiraterone decanoate-d17
0 ImagesCat. No.: HY-145786SAbiraterone decanoate-d17 is the deuterium labeled Abiraterone decanoate (HY-145786). Abiraterone decanoate is a potent Abiraterone proagent. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery.
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BNS808
0 ImagesBNS808 is an orally active and selective cannabinoid-1 receptor (CB1R) antagonist (IC50 = 0.8 nM) with notable CB2R selectivity and minimal brain penetration. BNS808 is studied in research on obesity and its associated metabolic complications, such as metabolic dysfunctional-associated steatotic liver disease (MASLD). BNS808 has reduced free drug availability for CNS entry, enhancing safety and minimizing drug-drug interactions through high plasma binding.
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Bergamottin (Standard)
0 ImagesSynonyms: 5-Geranoxypsoralen (Standard); Bergamotine (Standard); Bergaptin (Standard)Bergamottin (Standard) is the analytical standard of Bergamottin. This product is intended for research and analytical applications. Bergamottin is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
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SCYX-6759
0 ImagesCat. No.: HY-111906CAS No.: 1222509-12-7SCYX-6759 is an orally active, blood-brain barrier permeable anti-T. brucei agent. SCYX-6759 inhibits cytochrome P450 (IC50s: 30.3, 30.6, 47.4 μM for 2D6, 2C9, 2C19, respectively.) SCYX-6759 exhibits potent activity against T. b. brucei 427, T. b. rhodesiense STIB900, and T. b. gambiense STIB930, with IC50s of 0.07, 0.038 and 0.030 μg/mL, respectively.
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Adenosine receptor antagonist 6
0 ImagesCat. No.: HY-175195CAS No.: 2913578-04-6Adenosine receptor antagonist 6 is an orally active and selective A2A adenosine receptor (A2AAR) antagonist, with a Ki of 19.18 nM. Adenosine receptor antagonist 6 inhibits 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production (IC50 = 0.089 μM) and immunosuppression, while promoting IL-2 and IFN-γ secretion. Adenosine receptor antagonist 6 abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release. Adenosine receptor antagonist 6 inhibits tumor growth in a CT26/MC38 xenograft model. Adenosine receptor antagonist 6 can be used for the study of colon cancer.
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Fandosentan potassium
0 ImagesCat. No.: HY-105408ACAS No.: 221246-12-4Fandosentan potassium is a potent endothelin A receptor (ETAR) antagonist. Fandosentan potassium inhibits CYP2C9 and CYP3A4 activities with IC50 values of 39.6 and 21.6 μM, respectively. Fandosentan potassium reverses the hypoxic pulmonary vasoconstriction in the perinatal lamb. Fandosentan potassium can be used for pulmonary hypertension research[1][2].
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Casopitant
0 ImagesCat. No.: HY-14405CAS No.: 414910-27-3Synonyms: GW679769Casopitant (GW679769) is a potent, selective, brain-penetrant and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant antagonizes the emetic effects of Substance P (HY-P0201). Casopitant is also a substrate and weak to moderate inhibitor of CYP3A4. Casopitant is indicated for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
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Aromatase-IN-3
0 ImagesCat. No.: HY-162105Aromatase-IN-3 (compound 7d) is an aromatase inhibitor with an IC50 of 54 nM. Through suppressing the conversion of androstenedione to oestrogen caused by aromatase, Aromatase-IN-3 exerts an appreciable tumor growth inhibitory activities against breast cancer cell lines, suggesting its usage for ER+ cancer research.
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Sulfamethylphenazole
0 ImagesSulfamethylphenazole (Sulfapyrazole; Vesulong) is a long-acting sulfonamide antibacterial agent. Sulfamethylphenazole maintains effective chemotherapeutic blood concentrations through the slow release of free sulfonamide from a protein-binding reservoir and can be used in combination with antibiotics such as Terramycin for bovine hemorrhagic septicemia. Sulfamethylphenazole exhibits moderate antimycobacterial activity against Mycobacterium tuberculosis H37Rv (MIC = 15.38 μg/mL) and inhibitory activity against CYP 2C9. Sulfamethylphenazole can be used in studies related to tuberculosis and hemorrhagic septicemia.
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Dihydrocubebin
0 ImagesCat. No.: HY-N10421CAS No.: 24563-03-9Synonyms: (-)-DihydrocubebinDihydrocubebin is a compound isolated from Piper cubeba as potent and selective inhibitors against cytochrome P450 3A4 (CYP3A4).
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MK-5596
0 ImagesCat. No.: HY-10575CAS No.: 1044586-68-6MK-5596 is an efficient, selective and orally active CB1R (IC50 = 1.0 nM, EC50 = 5.8 nM) inverse agonist. MK-5596 has weak hERG inhibitory activity. MK-5596 has strong weight loss and appetite suppression effects. MK-5596 has a certain inhibitory effect on CYP enzymes (CYP3A4: IC50 = 3.3 μM, CYP2C8: IC50 = 11 μM, CYP2C9: IC50 = 18 μM, CYP2D6: IC50 = 6 μM). MK-5596 can be used for research on conditions such as obesity.
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CYP3A4-IN-6
0 ImagesCat. No.: HY-179011CYP3A4-IN-6 (Compound 8a) is a CYP3A4 inhibitor with tissue-selective metabolism. CYP3A4-IN-6 remains stable in the intestinal S9 component but is rapidly metabolized in the liver S9 component, forming a less active metabolite. CYP3A4-IN-6 can be used for intestinal selectivity studies.
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BI 653048 phosphate
0 ImagesCat. No.: HY-12946ACAS No.: 1198784-97-2BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM. BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM). BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus.
